Assay Detail
Binding
CHEMBL4605307
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Binding affinity to 6x-His-tagged human EphA2 ecto-domain residues (Lys27 to Asn529 residues) expressed in HEK293 cells incubated for 60 mins by fluorescence polarization assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.45 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642167 | — | — | 1 | 9.27 |
| CHEMBL4649686 | — | — | 1 | 8.82 |
| CHEMBL4641389 | — | — | 1 | 8.70 |
| CHEMBL4642849 | — | — | 1 | 8.55 |
| CHEMBL4634220 | — | — | 1 | 8.55 |
| CHEMBL4634551 | — | — | 1 | 8.51 |
| CHEMBL4636597 | — | — | 1 | 8.32 |
| CHEMBL4637644 | — | — | 1 | 8.29 |
| CHEMBL4643355 | — | — | 1 | 8.28 |
| CHEMBL4634880 | — | — | 1 | 8.26 |
| CHEMBL4640044 | — | — | 1 | 8.24 |
| CHEMBL4636032 | — | — | 1 | 8.24 |
| CHEMBL4648601 | — | — | 1 | 8.24 |
| CHEMBL4643893 | — | — | 1 | 8.17 |
| CHEMBL4637500 | — | — | 1 | 8.05 |
| CHEMBL4643498 | — | — | 1 | 7.89 |
| CHEMBL4635897 | — | — | 1 | 7.84 |
| CHEMBL4638336 | — | — | 1 | 7.58 |
| CHEMBL4642586 | — | — | 1 | 7.46 |
| CHEMBL4642437 | — | — | 1 | 7.41 |
| CHEMBL4644287 | — | — | 1 | 7.25 |
| CHEMBL4639187 | — | — | 1 | 7.09 |
| CHEMBL4645672 | — | — | 1 | 7.08 |
| CHEMBL4637860 | — | — | 1 | 7.08 |
| CHEMBL4647046 | — | — | 1 | 7.00 |
| CHEMBL4641388 | — | — | 1 | 6.94 |
| CHEMBL4638181 | — | — | 1 | 6.80 |
| CHEMBL4635141 | — | — | 1 | 6.68 |
| CHEMBL4645245 | — | — | 1 | 6.65 |
| CHEMBL4638393 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642167 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL4649686 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4641389 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4642849 | — | Ki | = | 2.83 | nM | 8.55 |
| CHEMBL4634220 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL4634551 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL4636597 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4637644 | — | Ki | = | 5.07 | nM | 8.29 |
| CHEMBL4643355 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL4634880 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4640044 | — | Ki | = | 5.78 | nM | 8.24 |
| CHEMBL4648601 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL4636032 | — | Ki | = | 5.74 | nM | 8.24 |
| CHEMBL4643893 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL4637500 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4643498 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL4635897 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL4638336 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL4642586 | — | Ki | = | 34.5 | nM | 7.46 |
| CHEMBL4642437 | — | Ki | = | 39.1 | nM | 7.41 |
| CHEMBL4644287 | — | Ki | = | 56.1 | nM | 7.25 |
| CHEMBL4639187 | — | Ki | = | 81.7 | nM | 7.09 |
| CHEMBL4645672 | — | Ki | = | 82.5 | nM | 7.08 |
| CHEMBL4637860 | — | Ki | = | 83.4 | nM | 7.08 |
| CHEMBL4647046 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL4641388 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4638181 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4635141 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4645245 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL4638393 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL4648501 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL4632996 | — | Ki | = | 539.0 | nM | 6.27 |
| CHEMBL4649266 | — | Ki | = | 815.0 | nM | 6.09 |
| CHEMBL4639176 | — | Ki | = | 931.0 | nM | 6.03 |
| CHEMBL4633239 | — | Ki | = | 2439.0 | nM | 5.61 |
| CHEMBL4637447 | — | Ki | = | 2618.0 | nM | 5.58 |
| CHEMBL4634115 | — | Ki | = | 3102.0 | nM | 5.51 |